Stable parenteral formulations of tigecycline
The invention relates to stable parenteral formulations of tigecycline and process of preparation thereof, wherein the formulation comprises an edetate, a pH modifying agent or an antioxidant, such that the formulation remains stable for at least 45 hours.
1. A stable parenteral formulation consisting of:
(a) tigecycline;
(b) an edetate;
(c) lactose monohydrate;
(d) sodium metabisulphite; and
(d) water for injection,
wherein the pH of the formulation prior to lyophilization is between 7.0 and 8.0.
2. The stable parenteral formulation of claim 1 , consisting of:
(a) 50 mg of tigecycline;
(b) 1 mg of an edetate;
(c) 100 mg of lactose monohydrate;
(d) 0.05 mg of sodium metabisulphite; and
(e) water.
3. The stable parenteral formulation of claim 1 , wherein the edetate is disodium edetate.
4. The stable parenteral formulation of claim 1 , wherein the tigecycline is present at 50 mg.
5. The stable parenteral formulation of claim 1 , wherein the edetate is present at 1 mg.
6. The stable parenteral formulation of claim 1 , wherein the lactose monohydrate is present at 100 mg.
7. The stable parenteral formulation of claim 1 , wherein the sodium metabisulphite is present at 0.05 mg.
8. The stable parenteral formulation of claim 1 , wherein the water is present in an amount sufficient to provide 1.5 ml for 50 mg of tigecycline.
9. The stable parenteral formulation according to claim 1 wherein the formulation does not degrade at least for 45 hours at 2° C. to 8° C.
10. The stable parenteral formulation according to claim 2 wherein the formulation does not degrade at least for 45 hours at 2° C. to 8° C.